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This combination led to mechanistic GPCR models that comprise both inactive and active-like receptor states.
Activity vs foulant weight data are compared to model predictions for both inactive and active fouling.
Among above, scaffold S1 and S6 were active in both NR1C1 and NR1C3 (Fig. 2d), while S8 and S9 were both inactive scaffold.
Therefore, we have built comparative models of the inactive and active conformations of the three receptors based on the three GPCRs for which structures of both inactive and fully active conformations were available at the time of the study.
In particular, activated GATA-1 induces two positive feedback loops in the system through the enhanced expression of both inactive GATA-1 and EpoR, the latter of which is externally regulatable by Epo.
6,6′-Diaminotrehalose and its diazido precursor were both inactive, but significant activity apparently related to aliphatic chain length was found among the sulfonamides, N-alkylamines, and one of the amidines.
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The results demonstrate that both the inactive and active states are present before phosphorylation, and activation occurs via a shift of this preexisting equilibrium.
Both the inactive (1F3M.PDB) and active conformations (1YHV.PDB) of Pak1 were utilized for analysis of Pak2 [21], [21].
The available crystal structures of other protein kinases in both the inactive and active states showed that the αC-helix is not always the key regulator of activity.
Both contain inactive kinase domains, as well as protein phosphatase and cNMP-binding domains.
RNAPII and H3K4me2/3 were present on both RS inactive genes and PS/RS inactive genes (Fig. 5b, d).
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